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Chemical Compound Review

Mifentidin     N-[4-(3H-imidazol-4- yl)phenyl]-N'-propan-2...

Synonyms: Mifentidina, Mifentidine, Mifentidinum, SureCN33303, CHEMBL308005, ...
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Disease relevance of DA 4577


High impact information on DA 4577


Chemical compound and disease context of DA 4577

  • A study has been done in 10 duodenal ulcer patients of the effect of a single oral dose of 10 mg mifentidine on the acid and pepsin responses to sham feeding after 1 h 30 min and to pentagastrin after 4 h 15 min [7].

Biological context of DA 4577


Anatomical context of DA 4577

  • Gastric acid and pepsin secretion after single oral doses of mifentidine in healthy subjects [11].
  • In addition, we elucidate both chemical transformations and the in vitro metabolism of mifentidine using guinea pig hepatic microsomes [12].
  • On the whole DA 4577 appeared to be a very potent and selective H2 antagonist which, unlike other members of the family, is devoid of non-specific effect on human atrium and on motility of the gastrointestinal tract of different animal species [13].
  • The present study, in which the degree of pseudo-irreversible H2-antagonism of the four isomeric butyl substituted mifentidine analogues was determined on the spontaneously beating right atrium of the male guinea-pig, lends further support to this hypothesis [14].
  • Two sets of experiments were performed: in the first, concerning the specific H2-receptor antagonism, DA 4577 was found to be extremely potent on the guinea-pig papillary muscle and on the human atrium stimulated by histamine (pA2 = 8.24 and 8.60 respectively) [13].

Associations of DA 4577 with other chemical compounds


Gene context of DA 4577


Analytical, diagnostic and therapeutic context of DA 4577

  • Therefore, in this animal model, mifentidine was about 40 times more potent than cimetidine and 5 times more potent than ranitidine [2].
  • In this work, we show the benefits of the high resolution capabilities of capillary electrophoresis (CE) and demonstrate that nonaqueous CE and on-line CE-mass spectrometry (CE-MS) leads to enhanced resolution and recovery of mixtures containing the prototype H2-antagonist, mifentidine, and putative metabolites [18].


  1. Comparative study of mifentidine and ranitidine in the short-term treatment of duodenal ulcer. Sabbatini, F., Lazzaroni, M., Petrillo, M., Piai, G., Mazzacca, G., Porro, G.B. Eur. J. Clin. Pharmacol. (1990) [Pubmed]
  2. The effect of the new H2-receptor antagonist mifentidine on gastric secretion, gastric emptying and experimental gastric and duodenal ulcers in the rat: comparison with cimetidine and ranitidine. Scarpignato, C., Tangwa, M., Tramacere, R., Del Soldato, P. Digestion (1986) [Pubmed]
  3. Safety and pharmacokinetics of mifentidine after increasing oral doses in healthy subjects. Imbimbo, B.P., Seiberling, M., Peuckert, U., Hoexter, G., Maier-Lenz, H., Vidi, A., Daniotti, S. Eur. J. Clin. Pharmacol. (1988) [Pubmed]
  4. Effect of the new H2-receptor antagonist mifentidine on gastric acid secretion in the cat: comparison with cimetidine and ranitidine. Scarpignato, C., Tramacere, R., Tangwa, M., Bertaccini, G. Archives internationales de pharmacodynamie et de thérapie. (1985) [Pubmed]
  5. Pharmacokinetics of mifentidine after single and multiple oral administration to healthy volunteers. Imbimbo, B.P., Urso, R., Thieme, G., Sturn, B., Ueckert, B., Vidi, A., Ladinsky, H., Daniotti, S. British journal of clinical pharmacology. (1988) [Pubmed]
  6. Inhibitory effects of H2-receptor antagonists on cytochrome P450 in male ICR mice. Kim, D.H., Kim, E.J., Han, S.S., Roh, J.K., Jeong, T.C., Park, J.H. Human & experimental toxicology. (1995) [Pubmed]
  7. Action of mifentidine on the secretory response to sham feeding and pentagastrin and on serum gastrin in duodenal ulcer patients. Bianchi Porro, G., Lazzaroni, M., Imbimbo, B.P., Sangaletti, O., Ghirardosi, C., Daniotti, S. Eur. J. Clin. Pharmacol. (1987) [Pubmed]
  8. Pharmacological profile of mifentidine: a novel H2-receptor antagonist. Giachetti, A., Pagani, F., Micheletti, R., Brambilla, A., Cereda, E., Donetti, A. Agents Actions (1985) [Pubmed]
  9. Pharmacology of mifentidine, a novel H2-receptor antagonist. Pagani, F., Micheletti, R., Brambilla, A., Schiavone, A., Montagna, E., Ciprandi, C., Giachetti, A. Arzneimittel-Forschung. (1985) [Pubmed]
  10. Effect of mifentidine on histamine-stimulated human atrium "in vitro": comparison with ranitidine and cimetidine. Poli, E., Medici, D., Contini, G.A., Bertaccini, G. Archives internationales de pharmacodynamie et de thérapie. (1985) [Pubmed]
  11. Gastric acid and pepsin secretion after single oral doses of mifentidine in healthy subjects. Lazzaroni, M., Imbimbo, B.P., Sangaletti, O., Bianchi Porro, G. Scand. J. Gastroenterol. (1988) [Pubmed]
  12. Investigation of the in vitro metabolism of the H2-antagonist mifentidine by on-line capillary electrophoresis-mass spectrometry using non-aqueous separation conditions. Tomlinson, A.J., Benson, L.M., Gorrod, J.W., Naylor, S. J. Chromatogr. B, Biomed. Appl. (1994) [Pubmed]
  13. Action of the new H2-antagonist, DA 4577, on different in vitro and in vivo preparations. Bertaccini, G., Poli, E., Coruzzi, G. Agents Actions (1984) [Pubmed]
  14. Irreversible H2-antagonism of the four isomeric butyl analogues of mifentidine. Bastiaans, H.M., Donetti, A., Kramer, K., Bietti, G., Cereda, E., Dubini, D., Mondini, M., Bast, A., Timmerman, H. Agents Actions (1990) [Pubmed]
  15. Cimetidine, ranitidine and mifentidine in specific gastric and duodenal ulcer models. Del Soldato, P., Ghiorzi, A., Cereda, E., Donetti, A. Pharmacology (1985) [Pubmed]
  16. Conformational studies of two histamine H2-receptor antagonistic phenylformamidines: mifentidine and its guanidinothiazole analogue DA 4643. Donetti, A., Trummlitz, G., Bietti, G., Cereda, E., Bazzano, C., Wagner, H.U. Arzneimittel-Forschung. (1985) [Pubmed]
  17. Action of mifentidine and ranitidine on the isolated rat uterus. Poli, E., Coruzzi, G., Bertaccini, G. Pharmacological research communications. (1984) [Pubmed]
  18. Capillary electrophoresis and capillary electrophoresis-mass spectrometry in drug and metabolite analysis. Naylor, S., Tomlinson, A.J., Benson, L.M., Gorrod, J.W. European journal of drug metabolism and pharmacokinetics. (1994) [Pubmed]
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